反应详情

A mixture of 2-(6-chloro-1-methyl-1H-indazol-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid (0.07 g, 0.3 mmol), pyridin-3-amine (0.05 g, 0.53 mmol), EDCI (0.057 g, 0.3 mmol), DMAP (0.037 g, 0.3 mmol), and DIPEA (0.163 g, 1.26 mmol) in 10 mL of DMF were stirred at room temperature for 5 hours. Then HATU (0.114 g, 0.3 mmol) was added, the final reaction mixture was stirred for additional. The solvent was removed under reduced pressure at 70° C. The residue was triturated with water, EtOAc and DMSO successively then decanted and dried to give 2-(6-chloro-1-methyl-1H-indazol-3-yl)-N-(pyridin-3-yl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxamide (0.022 g, 26%) as a white solid. MS: (M+H)+=404; 1H NMR (300 MHz, DMSO): δ 10.20 (s, 1H), 9.09 (s, 1H), 8.90 (s, 1H), 8.63 (s, 1H), 8.54 (d, 1H, J=8.7 Hz), 8.34 (d, 1H, J=4.5 Hz), 8.26 (d, 1H, J=8.7 Hz), 7.98 (s, 1H), 7.47 (dd, 1H, J=8.4, 4.8 Hz), 7.22 (d, 1H, J=8.4 Hz), 4.17 (s, 3H).

1. customthe final reaction mixture
2. stirringwas stirred for additional
3. customThe solvent was removed under reduced pressure at 70° C
4. customThe residue was triturated with water, EtOAc and DMSO successively
5. customdecanted
6. customdried